[Stability of amphetaminil. 2. In vivo studies]

The metabolism of radioactively labelled alpha-phenyl-alpha-N-(beta-phenyl-isopropyl)-aminoacetonitrile (amphetaminil, AN 1-R) (tritium-labelled in the amphetamine-part, 14C-labelled in the benzaldehyde-part of the molecule) in the rat was examined. In the body amphetaminil is cleft very quickly into the original compounds of its chemical synthesis (amphetamine, benzaldehyde and hydrocyanic acid) independent of the mode of application (i.p. or oral). Blood: In the interval from 5-90 min after application of amphetaminil only 1-2 percent of the total radioactivity are received from amphetaminil. The main part of the tritium- and 14C-radioactivity is distributed among amphetamine, p-OH-amphetamineglucuronide and hippuric acid. Brain: In the brain only a minimum amount of amphetaminil can be present, if any. The share of amphetamine of the total activity amounts to more than 90 percent. Adipose tissue: In the adipose tissue the ratio of the two isotopes of the substances extracted at pH 5 is almost equal to that of the administered amphetaminil. It seems that the substance is enriched there because of its pronounced lipophilia. After i.p. application the concentration is about 12 times higher than after oral application. Urine: In the urine there could be detected amphetamine, p-OH-amphetamineglucuronide and hippuric acid but no amphetaminil.